Abstract

Curcumin, extracted from the rhizome of Curcuma longa, has been widely used in medicine for centuries due to its anti-inflammatory, anti-cancer, anti-oxidant and anti-microbial effects. However, its bioavailability during treatments is poor because of its low solubility in water, slow dissolution rate and rapid intestinal metabolism. For these reasons, improving the therapeutic efficiency of curcumin using nanocarriers (e.g., biopolymer nanoparticles) has been a research focus, to foster delivery of the curcumin inside cells due to their small size and large surface area. Silk fibroin from the Bombyx mori silkworm is a biopolymer characterized by its biocompatibility, biodegradability, amphiphilic chemistry, and excellent mechanical properties in various material formats. These features make silk fibroin nanoparticles useful vehicles for delivering therapeutic drugs, such as curcumin. Curcumin-loaded silk fibroin nanoparticles were synthesized using two procedures (physical adsorption and coprecipitation) more scalable than methods previously described using ionic liquids. The results showed that nanoparticle formulations were 155 to 170 nm in diameter with a zeta potential of approximately −45 mV. The curcumin-loaded silk fibroin nanoparticles obtained by both processing methods were cytotoxic to carcinogenic cells, while not decreasing viability of healthy cells. In the case of tumor cells, curcumin-loaded silk fibroin nanoparticles presented higher efficacy in cytotoxicity against neuroblastoma cells than hepatocarcinoma cells. In conclusion, curcumin-loaded silk fibroin nanoparticles constitute a biodegradable and biocompatible delivery system with the potential to treat tumors by local, long-term sustained drug delivery.

Highlights

  • The yellow-orange compound 1,7-bis(4-hydroxy-3-methoxyphenyl)-1,6-heptadiene-3,5-dione (Figure S1), popularly known as curcumin, is the main phenolic pigment extracted from turmeric, the powdered rhizome of Curcuma longa, which comprises, approximately, 2–5% of turmeric [1]

  • The SF nanoparticles (SFNs), Curc-SFNs 1 and Curc-SFNs 2 were characterized by Dynamic Light Scattering (DLS) to ascertain their

  • Duryena1msihc oLwighsttShceatsteizriengan(DdLtSh) e Zeta Potential distributions of the SFNs and the Curc-SFNs obtained byTbhoetShFNmse, Cthuorcd-SsF.Ns 1 and Curc-SFNs 2 were characterized by DLS to ascertain their hydrodynamic diameter, Polidispersity Index (PdI), Zeta Potential and Electrophoretic Mobility (Table 1)

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Summary

Introduction

The yellow-orange compound 1,7-bis(4-hydroxy-3-methoxyphenyl)-1,6-heptadiene-3,5-dione (Figure S1), popularly known as curcumin, is the main phenolic pigment extracted from turmeric, the powdered rhizome of Curcuma longa, which comprises, approximately, 2–5% of turmeric [1]. Curcumin possesses remarkable medicinal benefits and has been safe, non-toxic and well-tolerated in animal and human studies, it cannot be administered to patients directly due to its poor solubility in water [1,16,19] (estimated value: 3.12 mg/L at 25 ◦C [20]). For this reason, the bioavailability of curcumin is limited due to of its reduced absorption. Research interests focus on the use of biopolymers, which are regarded as biodegradable, natural and environmentally friendly, to encapsulate curcumin and other similar drugs [27,42]

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